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Maikel Wijtmans

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Articles 63
Citations 621
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Recent Articles
1.
Berenger S, Adamska J, Deflorian F, de Graaf C, Palmer C, Szpakowska M, et al.
ACS Omega . 2025 Mar; 10(8):8675-8686. PMID: 40060784
Photopharmacology offers the promise of optical modulation of cellular signaling in a spatially and temporally controlled fashion with light-sensitive molecules. This study presents the first small-molecule photoswitchable agonist for an...
2.
Kuhne S, Bosma R, Kooistra A, Riemens R, Stroet M, Vischer H, et al.
J Med Chem . 2024 Dec; 68(1):448-464. PMID: 39723903
Analysis of structure-kinetic relationships (SKR) can contribute to an improved understanding of receptor-ligand interactions. Here, fragment (4-(2-benzylphenoxy)-1-methylpiperidine) was used in different fragment growing approaches to mimic the putative binding mode...
3.
Blaazer A, Singh A, Zara L, Boronat P, Bautista L, Irving S, et al.
ChemMedChem . 2024 Aug; 19(22):e202400417. PMID: 39193819
In search of new opportunities to develop Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitors that have selectivity over the off-target human PDE4 (hPDE4), different stages of a fragment-growing campaign were studied...
4.
Shi S, Zheng Y, Goulding J, Marri S, Lucarini L, Konecny B, et al.
Biochem Pharmacol . 2024 Jun; 226:116396. PMID: 38942089
This study introduces (S)-Opto-prop-2, a second-generation photoswitchable ligand designed for precise modulation of β-adrenoceptor (βAR). Synthesised by incorporating an azobenzene moiety with propranolol, (S)-Opto-prop-2 exhibited a high PSS (photostationary state...
5.
Zheng Y, Gao M, Wijtmans M, Vischer H, Leurs R
Pharmaceuticals (Basel) . 2024 Apr; 17(4). PMID: 38675496
The modulation of biological processes with light-sensitive chemical probes promises precise temporal and spatial control. Yet, the design and synthesis of suitable probes is a challenge for medicinal chemists. This...
6.
Zarca A, Adlere I, Viciano C, Arimont-Segura M, Meyrath M, Simon I, et al.
Mol Pharmacol . 2024 Feb; 105(4):301-312. PMID: 38346795
Atypical chemokine receptor 3 (ACKR3), formerly referred to as CXCR7, is considered to be an interesting drug target. In this study, we report on the synthesis, pharmacological characterization and radiolabeling...
7.
Simon I, Homan E, Wijtmans M, Sundstrom M, Leurs R, de Esch I, et al.
J Chem Inf Model . 2023 Oct; 63(21):6696-6705. PMID: 37831965
Photoswitchable (PSW) molecules offer an attractive opportunity for the optical control of biological processes. However, the successful design of such compounds remains a challenging multioptimization endeavor, resulting in several biological...
8.
FitzGerald E, Vagrys D, Opassi G, Klein H, Hamilton D, Talibov V, et al.
SLAS Discov . 2023 Sep; 29(1):40-51. PMID: 37714432
Surface plasmon resonance (SPR) biosensor methods are ideally suited for fragment-based lead discovery.  However, generally applicable experimental procedures and detailed protocols are lacking, especially for structurally or physico-chemically challenging targets...
9.
Dekker T, Janssen M, Sutherland C, Aben R, Scheeren H, Blanco-Ania D, et al.
ACS Med Chem Lett . 2023 May; 14(5):583-590. PMID: 37197454
The recent success of fragment-based drug discovery (FBDD) is inextricably linked to adequate library design. To guide the design of our fragment libraries, we have constructed an automated workflow in...
10.
Dekker T, W Harteveld J, Wagner G, de Vries M, Custers H, van de Stolpe A, et al.
Molecules . 2023 Feb; 28(4). PMID: 36838763
Biomass-derived molecules can provide a basis for sustainable drug discovery. However, their full exploration is hampered by the dominance of millions of old-fashioned screening compounds in classical high-throughput screening (HTS)...